In vitro activity: STF-31 selectively kills RCCs by specifically targeting glucose uptake through GLUT1. STF-31 significantly inhibits lactate production and extracellular acidification in VHL-deficient cells by about 60%, and decreases glycolysis by decreasing glucose transport. In NAPRT1-expressing cells, STF-31 shows cytotoxicity by inhibiting the enzymatic activity of NAMPT. STF-31 is toxic to hPSCs and efficient for selective elimination of hPSCs from mixed cultures.

Kinase Assay: STF-31 is a novel potent and selective glucose transporter (GLUT1) inhibitor with IC50 of 1 μM. STF31 selectively kills RCCs by specifically targeting glucose uptake through GLUT1 and exploiting the unique dependence of these cells on GLUT1 for survival. Treatment with STF31 inhibits the growth of RCCs by binding GLUT1 directly and impeding glucose uptake in vivo without toxicity to normal tissue. STF-31 is toxic to hPSCs and efficient for selective elimination of hPSCs from mixed cultures.

Cell Assay: In NAPRT1-expressing cells, STF-31 shows cytotoxicity by inhibiting the enzymatic activity of NAMPT. STF-31 is toxic to hPSCs and efficient for selective elimination of hPSCs from mixed cultures.